Reaction Details |
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Target | Elongin-B/Elongin-C [17-112]/von Hippel-Lindau disease tumor suppressor [55-213] |
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Ligand | BDBM536268 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Fluorescence Polarization (FP) VHL Binding Assay |
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IC50 | 35400±n/a nM |
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Citation | Blaquiere, N; Dragovich, P; Gazzard, LJ; Pillow, T; Staben, ST; Wei, B; Xin, J (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof US Patent US11242344 Publication Date 2/8/2022 |
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More Info.: | Get all data from this article, Assay Method |
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Elongin-B/Elongin-C [17-112]/von Hippel-Lindau disease tumor suppressor [55-213] |
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Name: | Elongin-B/Elongin-C [17-112]/von Hippel-Lindau disease tumor suppressor [55-213] |
Synonyms: | VHL Elongin B/C complex |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 3 components. |
Component 1 |
Name: | von Hippel-Lindau disease tumor suppressor [55-213] |
Synonyms: | VHL | VHL (aa 55-213) | VHL_HUMAN |
Type: | Protein |
Mol. Mass.: | 18405.28 |
Organism: | Homo sapiens (Human) |
Description: | P40337[55-213] |
Residue: | 159 |
Sequence: | EAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRG
HLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPEN
YRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
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Component 2 |
Name: | Elongin-B |
Synonyms: | ELOB | ELOB_HUMAN | Elongin 18 kDa subunit | Elongin-B | RNA polymerase II transcription factor SIII subunit B | SIII p18 | TCEB2 | Transcription elongation factor B polypeptide 2 |
Type: | PROTEIN |
Mol. Mass.: | 13127.13 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_108414 |
Residue: | 118 |
Sequence: | MDVFLMIRRHKTTIFTDAKESSTVFELKRIVEGILKRPPDEQRLYKDDQLLDDGKTLGEC
GFTSQTARPQAPATVGLAFRADDTFEALCIEPFSSPPELPDVMKPQDSGSSANEQAVQ
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Component 3 |
Name: | Elongin-C [17-112] |
Synonyms: | ELOC | ELOC_HUMAN | TCEB1 | Transcription elongation factor B polypeptide 1 (aa 17-112) |
Type: | PROTEIN |
Mol. Mass.: | 10829.81 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 96 |
Sequence: | MYVKLISSDGHEFIVKREHALTSGTIKAMLSGPGQFAENETNEVNFREIPSHVLSKVCMY
FTYKVRYTNSSTEIPEFPIAPEIALELLMAANFLDC
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BDBM536268 |
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n/a |
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Name | BDBM536268 |
Synonyms: | (5S)-2-((4R)-4-hydroxy-1-(2-(3-hydroxyisoxazol-5- yl)-3-methylbutanoyl)pyrrolidin-2-yl)-5-methyl-5-(4- (4-methylthiazol-5-yl)phenyl)-1,5-dihydro-4H- imidazol-4-one | US11242344, Example 116.1 | US11242344, Example 116.2 | US11242344, Example 116.3 | US11242344, Example 116.4 |
Type | Small organic molecule |
Emp. Form. | C26H29N5O5S |
Mol. Mass. | 523.604 |
SMILES | CC(C)C(C(=O)N1C[C@H](O)CC1C1=NC(=O)[C@@](C)(N1)c1ccc(cc1)-c1scnc1C)c1cc(O)no1 |r,t:13| |
Structure |
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